In this article the synthesis, characterization, acute toxicity, and antitumor activity of the novel Ru3+ complex are described. Through the acute toxicity tests, it was possible to fit the complexes into categories according to the OECD protocol guideline 423. The cisplatin complex was classified in category 1 and the sodium diaquodimalonateruthenate(3+) - Na[Ru(H2O)2(Mal-κ2O)2] - was classified in category 4. This result demonstrates the lower toxicity achieved by the ruthenium complex in comparison with metallopharmaceuticals compound. Evaluations of tumor masses extracted from mice inoculated with Ehrlich ascites carcinoma demonstrated percent inhibition lowest to cisplatin. Cisplatin showed 58% inhibition (1 mg/kg), while Na[Ru(H2O)2(Mal-κ2O)2] complex (5 mg/kg) presented 77%.

The synthesis, characterization, cytotoxicity and antitumor activity of platinum(II) complexes coordinated to O-glycoside and analogous is reported. Through the acute toxicity tests, it was possible to fit the complexes into categories according to the OECD protocol. The cis-[PtCl2(C6H14S2O2)-κ2S] complex was classified in category 3 and the cis-[PtCl2(C26H38O12S2)-κ2S] complex was classified in category 4. This result demonstrates the lower toxicity achieved by the glycoside in comparison with its analogous system. Evaluations of tumor masses extracted from mice inoculated with Ehrlich carcinoma demonstrated percent inhibition similar to cisplatin and synthesized platinum complexes. Cisplatin showed 59% inhibition, while cis-[PtCl2(C6H14S2O2)-κ2S] and cis-[PtCl2(C26H38O12S2)-κ2S] complexes presented 57% and 59%, respectively. Although the glycosidic compounds exhibit tumor activity, reported in the literature, the presence of platinum ion was shown to be determinant for antitumor action according with the compounds tested, since the glycosidic ligand presented tumor inhibition of only 38%, with a similar antitumor activity in relation to cisplatin.

A modified and efficient Knoevenagel condensation procedure was developed to synthesize the title compounds using β-alanine and acetic acid as catalysts, showing good to excellent yields. We used lawsone with suitable aliphatic aldehydes including isobutyraldehyde, 3-methyl-butyraldehyde, 2-ethylbutyraldehyde, phenylacetaldehyde, 2-phenyl-propionaldehyde, among others. These compounds were submitted to cytotoxic screening against three tumor cell lines presenting good to excellent cytotoxic profiles.

ABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.

ABSTRACT Phoradendron mucronatum and P. microphyllum are plants that found in tropical and subtropical areas, used in traditional medicine and popularly known as mistle-thrush. The aim of this study was to identify the chemical constituents of different leaf extracts from P. mucronatum and P. microphyllum and assess cytotoxic activity against strains from a human tumour cells. Extracts obtained with hexane, dichloromethane, chloroform and ethyl acetate from the leaves were analysed by gas chromatography coupled with mass spectrometry (GC-MS) and the cytotoxicity was assessed by the MTT method (bromide (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)). The tested human tumour cells were NCI-H292 (human pulmonar mucoepidermoid carcinoma), MCF-7 (human breast adenocarcinoma) and HEp-2 (epidermoid carcinoma of the larynx). Analysis by GC/MS of the extracts from leaves of P. microphyllum and P. mucronatum detected 51 different compounds, such as alkaloids, diterpenes, triterpenes, sterols, alcohols, aldehydes, fatty acids and hydrocarbons. In the cytotoxic evaluation, hexane and ethyl acetate extracts from the leaves P. microphyllum inhibited cell growth of NCI-H292 strains (72.97%) and HEp-2 (87.53%), respectively. The extracts of P. mucronatum species showed an inhibitory effect towards NCI-H292 (83.19%/hexane), MCF-7 (88.69%/dichloromethane) and HEp-2 (93.40%/hexane). The extracts showed cytotoxic activity against the tested strains, especially the P. mucronatum, which presented the highest percentages of inhibition of cell growth.

Abstract Solanum paniculatum L., Solanaceae, locally known as "jurubeba", is widely used in Brazil for culinary purposes, and in folk medicine to treat of diverse disorder including gastric dysfunctions. In this study we investigated the antidiarrheal activity of S. paniculatum roots extract in rats at different concentrations (125, 250 and 500 mg/kg, p.o) using different experimental models such as castor oil-induced diarrhea, enteropooling and gastrointestinal motility, determined by in vivo experimental models. The major compound of root extract was characterized as chlorogenic acid based in the IR, 1D and 2D NMR analysis. All the extract doses achieved antidiarrheal potency, as indicated by reduced weight of feces in castor oil-induced diarrhea, decreased intestinal motility and significantly inhibited castor oil-induced enteropooling compared to the vehicle group. The highest dose (500 mg/kg) produced greater anti-motility effect and better reduction of enteropooling, similar to the reference drug Loperamide (5 mg/kg). Extract from S. paniculatum L. roots had antidiarrheal activity, as shown by the lower weight of the feces as well as decrease in the accumulation of intestinal fluid and slower transit, justifying the traditional use of plant for diarrhea.

Croton zehntneri (Euphorbiaceae) é uma planta aromática nativa da região Nordeste do Brasil. O monoterpenóide Estragol (ESL) foi isolado por métodos cromatográficos clássicos a partir do óleo essencial (OE) das folhas de C. zehntneri e caracterizado por CG-DIC e CG-EM, tendo seu potencial antimicrobiano e citotóxico avaliado. A análise do OE permitiu a identificação de 100% dos constituintes integrados, cujo rendimento foi cerca de 1.8%. Os principais componentes identificados foram: eucaliptol, estragol (84.7%) e espatulenol. A dosagem de 50 μg/disco de ESL apresentou halos de inibição bastante expressivos frente a bactérias gram positiva e fungos. O ESL apresentou toxicidade frente a Artemia salina com CL50 e CL90 de 4,54 e 8,47 μg mL-1. Entretanto, nos testes de inibição tumoral (células humanas), não houve inibição satisfatória em nenhuma das linhagens de células humanas cancerígenas (MCF-7, HEP-2 e NCIH292).

Croton zehntneri (Euphorbiaceae) is a native aromatic plant from Northeast region of Brazil. The monoterpenoid estragole (ESL) has been isolated by classical chromatographic methods from the essential oil (EO) of C. zehnteneri leaves and characterized by GC-FID and GC-MS, its antimicrobial and cytotoxic potentials being assessed. The analysis of the EO enabled the identification of 100% of the integrated constituents, of which yield was about 1.8%. The main components identified were: eucalyptol, estragole (84.7%) and spathulenol. The dosage of 50 μg/disk of ESL presented fairly significant zones of inhibition against Gram-positive bacteria and fungi. The ESL presented toxicity against Artemia salina with LC50 and LC90 of 4,54 and 8,47 μg mL-1. However, in tumor inhibition assays (human cells), there were no rewarding inhibition in any of the human cancer cell lines (MCF-7, HEP-2 and NCI-H292).

This paper presents an investigation on the cytotoxic activity in human tumor cell from dichloromethane, chloroform, methanol, ethanol, water extracts, and hexane and chloroform fractions from green, brown and red algae collected at Riacho Doce Beach, north coast of Alagoas, Brazil, against the cancer cells K562 (chronic myelocytic leukemia), HEp-2 (laryngeal epidermoid carcinoma) and NCI-H292 (human lung mucoepidermoid carcinoma) through the MTT colorimetric method. The dichloromethane extract and chloroform fraction of Hypnea musciformis showed the best cytotoxic activity against K562 (3.8±0.2 µg.mL-1 and 6.4±0.4 µg.mL-1, respectively). Dichloromethane extracts of Dictyota dichotoma (16.3±0.3 µg.mL-1) and the chloroform fraction of H. musciformis (6.0±0.03 µg.mL-1) and chloroform fraction of P. gymnospora (8.2±0.4) were more active against HEp-2 as well as ethanol extracts of P. gymnospora (15.9±2.8 µg.mL-1) and chloroform fraction of H. musciformis (15.0±1.3 µg.mL-1) against the cell NCI-H292. The constituents with higher anticancer action are present in the extracts of dichloromethane and chloroform and in the chloroform fraction of H. musciformis, Digenea simplex, P. gymnospora, and D.dichotoma. In the case of the seaweed S. vulgare, the anticancer constituents are present in the aqueous extract.

Due to its folk use, scientific reports and phytochemical screening, the purpose of this work was to study the phytochemical and the biological properties of the methanol extract and to evaluate the anti-inflammatory activity as well as determine the acute toxicity, antitumor and cytotoxic activity of the root barks of Guettarda platypoda DC., Rubiaceae. In this analysis the presence of flavonoids and therpenoids were identified. These data and the ones in the literature indicated it as a potential antioxidant and motivated the cytotoxic analysis related with three tumoral cell strains as well as to evaluate its antitumoral activity (sarcoma 180 and Ehrlich carcinoma) in female mice. Due to the presence of esteroids and the previous study of the ethanolic extract, its anti-inflammatory activity and toxicity were also evaluated. Absence or low toxicity in 2000 mg/kg doses was verified and the attention to their phytochemical and pharmacological properties is constantly increasing.

Cissus sicyoides pertence à família das Vitaceae. É conhecido popularmente como "insulina, cipó-puca, bejuco caro, puci, anil trepador". Esta planta apresenta efeito vasoconstritor eatividade antibacteriana. No Brasil, C. sicyoides foi avaliado pelas suas propriedades anticonvulsivante e anti-diabética. Estudos fitoquímicos identificaram e isolaram a partir de suas partes aéreas o sitoesterol e o resveratrol compostos que são apontados por apresentar atividade antitumoral. O objetivo deste estudo foi investigar as atividades citotóxica e antitumoral do extrato hidroalcoólico Cissus sicyoides bem como a sua capacidade de recrutar leucócitos para os tecidos lesados. Cissus sicyoides não demonstrou atividade citotóxica, mas apresentou uma inibição do crescimento tumoral frente aos tumores testados. O extrato teve um forte efeito quimiotático 24 h após o tratamento. O extrato hidroalcoólico de Cissus sicyoides apresentou atividade antitumoral, relacionada ao recrutamento de linfócitos T para o local da lesão sugerindo que esta atividade esteve relacionada à ativação da linhagem linfóide.

Cissus sicyoides L. pertains to the Vitaceae family. It is popularly known as "insulina, cipo-pucá, bejuco caro, puci, anil trepador". A vasoconstrictor effect and an antibacterial activity have also been allocated to it. In Brazil, C. sicyoides was evaluated for its anticonvulsant and anti-diabetc properties. Phytochemistry studies identified and isolated sitosterol and resveratrol compounds from its aerial parts which are pointed out as having antitumor activities. The goal of this study was to investigate the cytotoxic and antitumor activities of Cissus sicyoides hydroalcoholic extract as well as its ability to repair leukocytes cells to injured tissue. Cissus sicyoides did not demonstrate cytotoxic activity but showed an inhibition of tumor growth in face of the tumors tested. The extract had a strong chemotactic effect on the twenty four hours period after treatment. The hidroalchoolic extract of Cissus sicyoides presented antitumor activity which was prompted by T lymphocytes recruitment to the local lesion and suggests a new pathway to antitumor activity by activation of lymphoid lineage.